Synthesis and biological evaluation of novel curcumin analogues as anti-inflammatory, anti-cancer and anti-oxidant agents

The new series of asymmetrical pyrazole curcumin analogues 4a-g were synthesized by using polyethylene glycol (PEG-400) as a green reaction medium and evaluated for their in vivo analgesic and in vitro antioxidant (H2 O2 , DPPH, Ferrous reducing power and Nitric oxide scavenging activity) and anti-inflammatory activities. All the compounds synthesized 4a-g showed the potential to demonstrate analgesic activity as compared to the standard ibuprofen. Among the tested series, compounds 4e and 4b exhibited good hydrogen peroxide scavenging activity as compared to the standard butylated hydroxy toluene (BHT). Compounds 4b, 4d, 4f, and 4g showed good DPPH free radical scavenging activity. Compounds 4b, 4c, 4d, 4e and 4g showed excellent ferrous-reducing power activity, whereas all the compounds showed better nitric oxide scavenging activity than standard ascorbic acid. Additionally, all the synthesized compounds were also screened for their in vitro anti-inflammatory activity. Compounds 4b, 4d, 4f and 4g showed good anti-inflammatory activity as compared to standard diclofenac sodium.

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“…Bandgar et al . have also synthesized novel curcumin analogues and evaluated as anti‐inflammatory, anticancer and antioxidant agents.…”

Section: Methodsmentioning

confidence: 99%

PEG Mediated Synthesis and Biological Evaluation of Asymmetrical Pyrazole Curcumin Analogues as Potential Analgesic, Anti‐Inflammatory and Antioxidant Agents

et al. 2014

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“…40) has emerged as the most potent inhibitor with 75% inhibition at 10 mM and only 3-fold stronger than standard salicylic acid, amongst a series of chalcone-Mannich adducts [217]. Adopting a similar molecular design [218], a library of chalcone-benzamides were found with slightly improved potency and SAR analysis established the preference of EWGs over EDGs for better enzyme inhibition. Compound 142 containing similar 3-Br substituent as compound 141, emerged as the most potent molecule (84.68% inhibition at 1 mM); 3-fold stronger potency than salicylic acid (24.77% at 1 mM).…”

Section: Chalconesmentioning

confidence: 99%

Therapeutic significance of β-glucuronidase activity and its inhibitors: A review

Awolade

Cele

Kerru

et al. 2020

European Journal of Medicinal Chemistry

107

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BiomarkerEnzyme inhibition Molecular target Structure activity relationship a b s t r a c tThe emergence of disease and dearth of effective pharmacological agents on most therapeutic fronts, constitutes a major threat to global public health and man's existence. Consequently, this has created an exigency in the search for new drugs with improved clinical utility or means of potentiating available ones. To this end, accumulating empirical evidence supports molecular target therapy as a plausible egress and, b-glucuronidase (bGLU) e a lysosomal acid hydrolase responsible for the catalytic deconjugation of b-D-glucuronides has emerged as a viable molecular target for several therapeutic applications. The enzyme's activity level in body fluids is also deemed a potential biomarker for the diagnosis of some pathological conditions. Moreover, due to its role in colon carcinogenesis and certain drug-induced dose-limiting toxicities, the development of potent inhibitors of bGLU in human intestinal microbiota has aroused increased attention over the years. Nevertheless, although our literature survey revealed both natural products and synthetic scaffolds as potential inhibitors of the enzyme, only few of these have found clinical utility, albeit with moderate to poor pharmacokinetic profile. Hence, in this review we present a compendium of exploits in the present millennium directed towards the inhibition of bGLU. The aim is to proffer a platform on which new scaffolds can be modelled for improved bGLU inhibitory potency and the development of new therapeutic agents in consequential.

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“…curcumin is an all-natural compound extracted from plants. It has many biological activities including anti-inflammatory, anti-infective and immune-regulating, and it protects the intestinal mucosa and repairs the function of intestinal tissue (35,36). other similar studies have shown that in the DSS-induced colitis model, curcumin is found to significantly improve intestinal inflammation, repair the intestinal mucosa and inhibit the expression of TnF-α and p38MaPK (23,24).…”

Section: Discussionmentioning

confidence: 92%

Curcumin ameliorates DSS‑induced colitis in mice by regulating the Treg/Th17 signaling pathway

et al. 2020

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Synthesis and biological evaluation of novel curcumin analogues as anti-inflammatory, anti-cancer and anti-oxidant agents

Cited by 13 publications

References 33 publications

PEG Mediated Synthesis and Biological Evaluation of Asymmetrical Pyrazole Curcumin Analogues as Potential Analgesic, Anti‐Inflammatory and Antioxidant Agents

PEG Mediated Synthesis and Biological Evaluation of Asymmetrical Pyrazole Curcumin Analogues as Potential Analgesic, Anti‐Inflammatory and Antioxidant Agents

Therapeutic significance of β-glucuronidase activity and its inhibitors: A review

Curcumin ameliorates DSS‑induced colitis in mice by regulating the Treg/Th17 signaling pathway

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